Small-Molecule Anti-Cancer Drugs From 2016 to 2020: Synthesis and Clinical Application

Abstract

Malignant tumors have become a significant public health problem that severely threatens human health. Drug-targeting therapy is essential for tumor therapy, along with surgery and radiotherapy. Of the 378 novel drugs approved over the past five years, those for oncological therapy remains at the top (25%). These drugs are used to treat patients with various cancers by acting on corresponding targets, such as EGFR, JAK, BTK, IDH, and FLT3. This review examines anti-tumor agents approved between 2016 and 2020, classifying them according to indication (such as lung cancer, leukemia, breast cancer, and myeloma). These drugs are reviewed according to their route of administration, first-in-class designation, approval dates, and expedited review categories. Furthermore, this paper summarizes the targets and modes of action of the approved anti-tumor drugs while systematically discussing their synthetic routes for medicinal chemistry or industrial use, which will benefit next-generation drug discovery.